| 应用 |
A tyrosine kinase, c-Kit, PDGFR, FGFR3, the FAK pathway inhibitor. |
| 产品介绍 |
Masitinib (AB1010)是一种新型的Kit和PDGFRα/β抑制剂，IC50分别为200 nM和540 nM/800 nM，但对ABL和c-Fms抑制作用较弱。Phase 3 |
| 备注 |
Masitinib is a novel inhibitor for Kit and PDGFRα/β with IC50 of 200 nM and 540 nM/800 nM, weak inhibition to ABL and c-Fms. Phase 2/3. |
| 生化机理 |
Masitinib (AB1010) is a tyrosine kinase, c-Kit, PDGFR, FGFR3, the FAK pathway inhibitor with IC50 of 150 ± 80, 200 ± 40 nM for KIT tyrosine phosphorylation and the recombinant wild-type KIT. Masitinib can enhance the antiproliferative effects of gemcitabine (GEM) in pancreatic cancer cells. Masitinib potently inhibits KIT with activating mutations in the juxtamembrane domain. |
| 别名 |
马赛替尼;4-[(4-甲基-1-哌嗪基)甲基]-N-[4-甲基-3-[[4-(3-吡啶基)-2-噻唑基]氨基]苯基]苯甲酰胺;AB1010;Masivet;AB-1010;AB 1010;N-(4-methyl-3-(4-(pyridin-3-yl)thiazol-2-ylamino)phenyl)-4-((4-methylpiperazin-1-yl)methyl)benzamide;4-[(4-Methyl-1-piperazinyl)methyl]-N-[4-methyl-3-[[4-(3-pyridinyl)-2-thiazolyl]amino]phenyl]benzamide |
